Potency ratio between opioid agonists and partial agonists.

نویسنده

  • B Kay
چکیده

POTENCY RATIO BETWEEN OPIOID AGONISTS AND PARTIAL AGONISTS Sir,—The paper by Klepper and colleagues (1986) again seems to indicate the belief of this group of workers in a fixed potency ratio between opioid agonists and partial agonists, although such a concept is theoretically unlikely (Kay, 1985). Support for a variable potency ratio is apparent in their paper, however, in that nalbuphine in so-called "equipotent" doses smaller than those in the range (8-10 mg) where equipotency has been demonstrated (Beaver and Feise, 1978) produced a greater effect than morphine. This observation correlates with the theoretical prediction based on nalbuphine having a flatter dose-response relation than morphine, as docs the observation that doses of nalbuphine in excess of 10 mg produced less effect than "equipotent" doses of morphine. The paper confirms that nalbuphine has a flatter dose—response relation than morphine, and that a ceiling effect, or even reversal of effect, occurs. With non-parallel dose-response relations, any potency ratio between nalbuphine and morphine can only apply at a single dose.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Clocinnamox distinguishes opioid agonists according to relative efficacy in normal and morphine-treated rats trained to discriminate morphine.

High doses of insurmountable antagonists or frequent administration of high doses of agonists are required to alter the potency of opioid agonists to produce discriminative stimuli. In the present study, insurmountable antagonism and repeated agonist treatment were combined to remove or disable a large enough proportion of mu-opioid receptors to alter the potency or maximal effect for four agon...

متن کامل

The relative potency of inverse opioid agonists and a neutral opioid antagonist in precipitated withdrawal and antagonism of analgesia and toxicity.

Opioid antagonists can be classified as inverse agonists and neutral antagonists. In the opioid-dependent state, neutral antagonists are significantly less potent in precipitating withdrawal than inverse agonists. Consequently, neutral opioid antagonists may offer advantages over inverse agonists in the management of opioid overdose. In this study, the relative potency of three opioid antagonis...

متن کامل

Marketed New Drug Delivery Systems for Opioid Agonists/Antagonists ‎Administration: A Rapid Overview

Novel drug delivery systems for controlled-release of opioid agonists as a long time painkillers or opioid antagonists for opium, heroin, and alcohol addiction are under development or in clinical use today. In this article, the field of “new drug delivery systems” is momentarily reviewed from the viewpoint of the marketed opioid agonists/antagonists dosage forms today.

متن کامل

Opioid drugs as reinforcing stimuli in rhesus monkeys

Working in a laboratory at the University of Michigan that was originally designed in the 1960s by Dr. Tomoji Yanagita, we have been evaluating opioid drugs for their ability to maintain behavior in rhesus monkeys. The animals are prepared with intravenous catheters that can be accessed from the outside of the cage. Inside the cage are two response levers and several stimulus lights. When one o...

متن کامل

Signal transduction correlates of mu opioid agonist intrinsic efficacy: receptor-stimulated [35S]GTP gamma S binding in mMOR-CHO cells and rat thalamus.

This study examined the signal transduction correlates of mu opioid agonist efficacy in two systems: mu receptor-transfected mMOR-CHO cell and rat thalamic membranes. The potency and maximal stimulation of [35S]GTP gamma S binding by various agonists was measured in the presence of excess GDP and compared with receptor binding affinity under identical assay conditions. Results showed that the r...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • British journal of anaesthesia

دوره 59 6  شماره 

صفحات  -

تاریخ انتشار 1987